Mono Rum retard - instructions for use, dose, side effects, contraindications

Description:Capsules hard gelatinous № 2 reddish-brown color - for a dosage of 40 mg. Hard gelatin capsules No. 1 with a blue lid and a white body for a dosage of 60 mg. The contents of the capsules are pellets of white or almost white color.

Pharmacotherapeutic group:Vasodilating agent - nitrate

ATX: & nbsp

C.01.D.A.14 Isosorbide mononitrate

Pharmacodynamics:

Isosorbide mononitrate is a periphyrical vasodilator with a predominant effect on venous vessels. Has vasodilator and antianginal action. Reduces preload (by expanding peripheral veins) and postnagruzku (due to a decrease in the total peripheral vascular resistance), reduces the need for myocardium in oxygen,expands coronary arteries and improves coronary blood flow, promotes its redistribution into ischemic areas, reduces the terminal diastolic volume of the left ventricle and reduces the systolic tension of its walls.

Increases tolerance to physical activity in patients with coronary heart disease (CHD), reduces pressure in a small circle of blood circulation.

Isosorbide mononitrate causes relaxation of the musculature of the bronchi, urinary tract, gall bladder muscles, bile ducts and esophagus, as well as the small and large intestine, including sphincters.

At the molecular level, nitrates act through the formation of nitrogen (NO) oxide and cyclic guanosine monophosphate, which mediates the relaxation of the smooth muscles of the internal organs.

It dilates the vessels of the brain, the dura mater, which can be accompanied by a headache. Like other nitrates, cross tolerance is developing. After cancellation (interruption in treatment) sensitivity to it is quickly restored.

Antianginal effect manifests itself after 30 minutes and lasts 2-6 hours.

Pharmacokinetics:

After oral administration isosorbide mononitrate quickly and completely absorbed from the gastrointestinal tract (GIT). Bioavailability is between 90-100% and does not depend on food intake. The connection with blood plasma proteins is less than 4%.

The therapeutic concentration of isosorbide mononitrate in the blood is reached after 30 minutes and is 250 ng / ml, during the 4th hour-414 ng / ml, during the 12th hour - 199 ng / ml (ie, the concentration decrease is slow).

Concentration in the blood plasma is directly proportional to the dose taken. The time to reach the maximum concentration is 8 hours.

Isosorbide mononitrate is almost completely metabolized in the liver (not exposed to the "first pass" effect) with the formation of inactive metabolites by denitration to isosorbide or by conjugation with glucuronic acid and the formation of inactive 2-glucuronide.

It is excreted by the kidneys, mainly in the form of metabolites, 2% - unchanged.

The half-life is 4-5 hours.

Indications:

- Prevention of attacks of stable angina pectoris in patients with coronary heart disease, including after a previous myocardial infarction;

- treatment of chronic heart failure (as part of combination therapy).

Contraindications:

- Hypersensitivity to organic nitrates or other components of the drug;

- acute circulatory disturbances (shock, collapse);

- Acute myocardial infarction with severe arterial hypotension;

- cardiogenic shock, if a sufficiently high final diastolic pressure in the left ventricle is not provided by application within the aortic counterpulsation or by the introduction of agents that have a positive inotropic effect;

- toxic pulmonary edema;

- Anemia (severe form);

- severe arterial hypotension (systolic blood pressure (BP) less than 90 mm Hg, diastolic blood pressure less than 60 mm Hg);

- simultaneous administration of inhibitors of phosphodiesterase 5 (sildenafil, tadalafil, vardenafil, as they potentiate the hypotensive effect of nitrates);

- age under 18 years (effectiveness and safety not established);

- Patients with rare hereditary diseases: fructose intolerance and glucose / galactose absorption impairment syndrome or insufficiency of sucrose / isomaltase.

Carefully:

- Hypertrophic obstructive cardiomyopathy, constrictive pericarditis, cardiac tamponade;

- low filling pressure for acute myocardial infarction, left ventricular failure.Do not lower the systolic / diastolic blood pressure lower than 90 mmHg;

aortic and / or mitral stenosis;

- the tendency to orthostatic disorders of vascular regulation;

- with glaucoma (risk of increase in eye pressure);

- severe renal insufficiency;

- liver dysfunction (risk of development of methemoglobinemia);

- hemorrhagic stroke;

- hyperthyroidism;

- diseases accompanied by increased intracranial pressure;

- suffered craniocerebral injury;

- increased peristalsis of the gastrointestinal tract;

- Malabsorption syndrome.

Pregnancy and lactation:For safety reasons, MONOP ROM RETARD can be used during pregnancy and lactation only strictly according to the doctor's prescription, after a thorough evaluation of the benefits to the mother and the possible risk to the fetus and / or child, as there is insufficient data on its use in pregnant and lactating mothers. If the nursing mother still accepts MONO ROM RETARD, it is necessary to establish observation of the child for the development of possible undesirable effects from the use of the drug.

Dosing and Administration:

Inside, the capsules are swallowed whole, washed down with water.

Frequency of admission and duration of treatment are set individually by the doctor. Treatment is recommended to start with a dose of MONO ROM RETARD 40 mg once a day, if necessary - with a dose of MONO ROM RETARD 60 mg once a day.

In some cases, the dose can be increased to 2 capsules (80 mg) in 2 divided doses per day. To achieve the full therapeutic effect, the second capsule of MONO ROM RETARD 40 mg (at a daily dose of 80 mg) should be taken no later than 8 hours later.

The maximum daily dose is 120 mg.

Side effects:

From the cardiovascular system: at the beginning of treatment, a "nitrate" headache is possible; marked decrease in blood pressure; Orthostatic hypotension, accompanied by reflex tachycardia, inhibition, dizziness, weakness; rarely with severe arterial hypotension - increased symptoms of angina (paradoxical reaction); in some cases - collapse, sometimes with bradyarrhythmia and fainting.

From the digestive system: nausea, vomiting, there may be a sensation of slight burning of the tongue, dryness of the oral mucosa.

From the central nervous system: drowsiness, blurred vision, decreased ability to rapid mental and motor reactions (especially at the beginning of treatment).

Allergic reactions: possibly transient redness of the skin, skin rash.

Other: development of tolerance, as well as cross-tolerance with other nitro compounds with long-term continuous treatment with high doses of isosorbide mononitrate. To prevent a decrease or loss of efficacy, continuous intake of high doses of the drug should be avoided.

In some cases exfoliative dermatitis.

Overdose:

Symptoms: pronounced BP reduction with orthostatic vasodilation, reflex tachycardia and headache. There may be weakness, dizziness, skin hyperemia, nausea, vomiting, diarrhea. In the high dose (more than 20 mg / kg body weight), the appearance of methemoglobinemia, cyanosis, dyspnea and tachypnea is expected due to the formation of nitrite ions due to the metabolism of isosorbide mononitrate.

At very high doses of the drug, intracranial pressure may increase with cerebral symptoms. In chronic overdose, an increase in methemoglobin is detected.

Treatment: gastric lavage, reception of activated carbon.

With a pronounced decrease in blood pressure - give the patient a horizontal position with raised legs and carry out measures for replenishing the volume of circulating blood (BCC); in exceptional cases, to improve blood circulation, it is possible to carry out infusions of norepinephrine (noradrenaline) and / or dopamine.

The use of epinephrine (adrenaline) and related compounds is contraindicated.

With methemoglobinemia:

1. Ascorbic acid - 1 g inside or in the form of the sodium salt IV - 0.1-0.15 ml / kg 1% solution up to 50 ml,

2. Oxygenotherapy, hemodialysis, exchange blood transfusion.

Interaction:

When used simultaneously with other vasodilators, beta-blockers, angiotensin converting enzyme (ACE) inhibitors, slow calcium channel blockers (BCCs), diuretics, neuroleptics, tricyclic antidepressants, ethanol, phosphodiesterase 5 inhibitorssildenafil, vardeafil, tadapafil), it is possible to intensify the antihypertensive effect of MONO ROM RETARD. With simultaneous application with dihydroergotamine, an increase in the concentration of dihydroergotamine in the blood plasma is possible.

Reduces the effect of vasopressors.

The therapeutic effect of norepinephrine (norepinephrine) decreases with simultaneous use with nitrosozedneniyami.

Barbiturates accelerate metabolism and reduce the concentration of isosorbide mononitrate in the blood plasma.

When combined with amiodarone, propranolol, BCCC (verapamil, nifedipine, etc.), it is possible to increase the antianginal effect.

Adsorbents, astringents and enveloping agents reduce the absorption of isosorbide mononitrate from the gastrointestinal tract.

When used simultaneously with m-holinoblokatorami (atropine and others), the risk of increasing intraocular pressure increases.

Under the influence of beta-adrenomimetics, alpha-adrenoblockers (dihydroergotamine and others), it is possible to reduce the antianginal effect (tachycardia and excessive BP decrease).

Special instructions:

The drug MONO ROM ROM RETARD should not be used to stop acute attacks of angina and acute myocardial infarction!

During the period of therapy with MONO ROM RETARD, control of blood pressure and heart rate is necessary.

It should be avoided abrupt withdrawal of the drug (dose gradually reduce).

With long-term use, the development of tolerance is possible, in connection with which,it is recommended to cancel for 24-48 hours or after 3-6 weeks of regular intake of the drug to take a break for 3-5 days, replacing the preparation MONO ROM RETARD with other antianginal drugs for this time.

The use of MONO ROM ROM RETARD can lead to transient hypoxemia due to the redistribution of blood flow to the hypoventilation alveolar segments. This may be the trigger mechanism of ischemia in patients with ischemic heart disease.

During the treatment should be excluded from the use of ethanol (alcohol).

Effect on the ability to drive transp. cf. and fur:During treatment with MONO ROM, RETARD is not recommended to drive vehicles and engage in potentially dangerous activities requiring a fast psychomotor reaction.

Form release / dosage:Capsules of prolonged action of 40 mg and 60 mg.

Packaging:10 capsules in a contour cell box made of polyvinylchloride film and aluminum foil. 2 contour mesh packages together with the instruction but put into a cardboard box.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children!

Shelf life:

3 years.

Do not use after the expiration date stated on the package!

Terms of leave from pharmacies:On prescription

Registration number:LSR-003091/10

Date of registration:12.04.2010

Expiration Date:Unlimited

The owner of the registration certificate:K.O. Ромфарм Компани С.Р.Л.K.O. Ромфарм Компани С.Р.Л. Romania

Manufacturer: & nbsp

S.C. ROMPHARM Company, S.R.L. Romania

Representation: & nbspРомфарма ОООРомфарма ООО

Information update date: & nbsp13.06.2018

Illustrated instructions

Instructions

Mono Rum retard (Mono Rom retard)